Literature DB >> 12657276

Inhibition of telomerase by BIBR 1532 and related analogues.

D K Barma1, Anissa Elayadi, J R Falck, David R Corey.   

Abstract

BIBR 1532 has been reported to be a potent, small molecule inhibitor of human telomerase, suggesting it as a lead for the development of anti-telomerase therapy. We confirm the ability of BIBR 1532 to inhibit telomerase and report the discovery of an equally potent analogue. Importantly, IC(50) values in cell extract are considerably higher than those previously reported using assays for purified enzyme, indicating that substantial improvement may be necessary.

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Year:  2003        PMID： 12657276     DOI： 10.1016/s0960-894x(03)00101-x

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  9 in total

Review 1.  Friend or foe? Telomerase as a pharmacological target in cancer and cardiovascular disease.

Authors:  Karima Ait-Aissa; Johnathan D Ebben; Andrew O Kadlec; Andreas M Beyer
Journal:  Pharmacol Res       Date:  2016-07-06       Impact factor: 7.658

2.  Targeting human telomerase for cancer therapeutics.

Authors:  Lionel Guittat; Patrizia Alberti; Dennis Gomez; Anne De Cian; Gaëlle Pennarun; Thibault Lemarteleur; Chafke Belmokhtar; Rajaa Paterski; Hamid Morjani; Chantal Trentesaux; Eliane Mandine; François Boussin; Patrick Mailliet; Laurent Lacroix; Jean-François Riou; Jean-Louis Mergny
Journal:  Cytotechnology       Date:  2004-06       Impact factor: 2.058

3.  Identification of an RNA aptamer binding hTERT-derived peptide and inhibiting telomerase activity in MCF7 cells.

Authors:  Akhil Varshney; Jyoti Bala; Baby Santosh; Ashima Bhaskar; Suresh Kumar; Pramod K Yadava
Journal:  Mol Cell Biochem       Date:  2016-12-21       Impact factor: 3.396

4.  Facile synthesis of naphthoquinone spiroketals by diastereoselective oxidative [3 + 2] cycloaddition.

Authors:  Kun-Liang Wu; Stephanie Wilkinson; Norbert O Reich; Thomas R R Pettus
Journal:  Org Lett       Date:  2007-11-29       Impact factor: 6.005

5.  Telomerase inhibition by siRNA causes senescence and apoptosis in Barrett's adenocarcinoma cells: mechanism and therapeutic potential.

Authors:  Masood A Shammas; Hemanta Koley; Ramesh B Batchu; Robert C Bertheau; Alexei Protopopov; Nikhil C Munshi; Raj K Goyal
Journal:  Mol Cancer       Date:  2005-07-15       Impact factor: 27.401

6.  Discovery of (4-bromophenyl)(3-hydroxy-4-methoxyphenyl)methanone through upregulating hTERT induces cell apoptosis and ERS.

Authors:  Xiu Cheng; Jing Bo Shi; Hao Liu; Liu Zeng Chen; Yang Wang; Wen Jian Tang; Xin Hua Liu
Journal:  Cell Death Dis       Date:  2017-08-24       Impact factor: 8.469

7.  Ethenesulfonyl fluoride derivatives as telomerase inhibitors: structure-based design, SAR, and anticancer evaluation in vitro.

Authors:  Xing Chen; Gao-Feng Zha; Jie Quan Wang; Xin-Hua Liu
Journal:  J Enzyme Inhib Med Chem       Date:  2018-12       Impact factor: 5.051

8.  Telomere elongation through hTERT immortalization leads to chromosome repositioning in control cells and genomic instability in Hutchinson-Gilford progeria syndrome fibroblasts, expressing a novel SUN1 isoform.

Authors:  Mehmet U Bikkul; Richard G A Faragher; Gemma Worthington; Peter Meinke; Alastair R W Kerr; Aakila Sammy; Kumars Riyahi; Daniel Horton; Eric C Schirmer; Michael Hubank; Ian R Kill; Rhona M Anderson; Predrag Slijepcevic; Evgeny Makarov; Joanna M Bridger
Journal:  Genes Chromosomes Cancer       Date:  2019-01-07       Impact factor: 5.006

9.  New Genetic Bomb Trigger: Design, Synthesis, Molecular Dynamics Simulation, and Biological Evaluation of Novel BIBR1532-Related Analogs Targeting Telomerase against Non-Small Cell Lung Cancer.

Authors:  Haytham O Tawfik; Anwar A El-Hamaky; Eman A El-Bastawissy; Kirill A Shcherbakov; Alexander V Veselovsky; Yulia A Gladilina; Dmitry D Zhdanov; Mervat H El-Hamamsy
Journal:  Pharmaceuticals (Basel)       Date:  2022-04-14
  9 in total

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